Preliminary evaluation of 1'-[(18)F]fluoroethyl-β-D-lactose ([(18)F]FEL) for detection of pancreatic cancer in nude mouse orthotopic xenografts

Nucl Med Biol. 2014 Nov-Dec;41(10):833-40. doi: 10.1016/j.nucmedbio.2014.08.001. Epub 2014 Aug 8.

Abstract

Introduction: Early detection of pancreatic cancer could save many thousands of lives. Non-invasive diagnostic imaging, including PET with [(18)F]FDG, has inadequate resolution for detection of small (2-3 mm) pancreatic tumours. We demonstrated the efficacy of PET imaging with an (18)F-labelled lactose derivative, [(18)F]FEDL, that targets HIP/PAP, a biomarker that is overexpressed in the peritumoural pancreas. We developed another analogue, 1-[(18)F]fluoroethyl lactose ([(18)F]FEL), which is simpler to synthesise, for the same application. We conducted a preliminary evaluation of the new probe and its efficacy in detecting orthotopic pancreatic carcinoma xenografts in mice.

Methods: Xenografts were developed in nude mice by injecting L3.6 pl/GL(+) pancreatic carcinoma cells into the pancreas of each mouse. Tumour growth was monitored by bioluminescence imaging (BLI); accuracy of BLI tumour size estimates was verified by MRI in two representative mice. When the tumour size reached approximately 2-3mm, the animals were injected with [(18)F]FEL (3.7 MBq) and underwent static PET/CT scans. Blood samples were collected at 2, 5, 10, 20 and 60 min after [(18)F]FEL injection to track blood clearance. Following imaging, animals were sacrificed and their organs and tumours/pancreatic tissue were collected and counted on a gamma counter. Pancreas, including tumour, was frozen, sliced and used for autoradiography and immunohistochemical analysis of HIP/PAP expression.

Results: Tumour growth was rapid, as observed by BLI and MRI. Blood clearance of [(18)F]FEL was bi-exponential, with half-lives of approximately 3.5 min and 40 min. Mean accumulation of [(18)F]FEL in the peritumoural pancreatic tissue was 1.29±0.295 %ID/g, and that in the normal pancreas of control animals was 0.090±0.101 %ID/g. [(18)F]FEL was cleared predominantly by the kidneys. Comparative analysis of autoradiographic images and immunostaining results demonstrated a correlation between [(18)F]FEL binding and HIP/PAP expression.

Conclusion: [(18)F]FEL may be useful for non-invasive imaging of early-stage pancreatic tumours by PET. The results warrant further studies.

Keywords: HIP/PAP; PET; Pancreatic cancer; Tumour imaging; [(18)F]lactose.

Publication types

  • Evaluation Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Female
  • Fluorine Radioisotopes* / pharmacokinetics
  • Humans
  • Immunoenzyme Techniques
  • Lactose / analogs & derivatives*
  • Lactose / pharmacokinetics
  • Lactose / pharmacology
  • Luminescent Measurements
  • Magnetic Resonance Imaging
  • Mice
  • Mice, Nude
  • Pancreatic Neoplasms / diagnosis*
  • Pancreatic Neoplasms / metabolism
  • Pancreatitis-Associated Proteins
  • Positron-Emission Tomography
  • Proteins / metabolism
  • Radiopharmaceuticals* / pharmacokinetics
  • Tissue Distribution
  • Tomography, X-Ray Computed
  • Tumor Cells, Cultured
  • Xenograft Model Antitumor Assays

Substances

  • 1'-fluoroethyllactose
  • Fluorine Radioisotopes
  • Pancreatitis-Associated Proteins
  • Proteins
  • REG3A protein, human
  • Radiopharmaceuticals
  • Reg3b protein, mouse
  • Lactose